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1.
Pharm Dev Technol ; 24(6): 729-738, 2019 Jul.
Article in English | MEDLINE | ID: mdl-30775948

ABSTRACT

Fennel (Foeniculum vulgare Mill.) is a member of family Apiaceae. Trans-anethole, the major component of Fennel essential oil (FEO), possesses antioxidant and hepatoprotective effects. Transdermal nanoemulsions (NEs) are advanced colloidal systems for systemic and controlled drug delivery through the stratum corneum barrier. FEO NEs were prepared using the oil Lauroglycol™ 90, as it provides a larger NE existence zone than Captex® 300, in the constructed phase diagrams. Six systems were prepared using Tween20/propylene glycol (S/CoS) in the ratios 2:1 and 3:1 with oil to S/CoS mass ratios 1:9, 2:8 and 3:7. Physicochemical characterization revealed optimum properties regarding thermodynamic stability, droplet size and pH with a Newtonian flow pattern. In vitro permeation study in rat skin revealed the highest cumulative amount permeated (µg/cm2), flux and permeability coefficient values for F4 made up of 2% FEO, 4.67% Lauroglycol™ 90, 60% S/CoS in the ratio 3:1. Results of the in vivo hepatic dysfunction study in rats indicate promising significant amelioration of liver function reflected in ALT, AST, ALP, bilirubin, albumin, malondialdehyde and ammonia plasma levels. The results signify the promising approach of FEO NEs in achieving remedy of liver toxicity. The most promising effect is inherent to F4 which imparts a more positive effect than FEO.


Subject(s)
Delayed-Action Preparations/chemistry , Foeniculum/chemistry , Liver Diseases/drug therapy , Oils, Volatile/administration & dosage , Oils, Volatile/therapeutic use , Administration, Cutaneous , Animals , Emulsions/chemistry , Liver/drug effects , Liver/physiopathology , Liver Diseases/physiopathology , Male , Oils, Volatile/chemistry , Oils, Volatile/pharmacokinetics , Polysorbates/chemistry , Propylene Glycol/chemistry , Rats , Skin Absorption
2.
Drug Dev Ind Pharm ; 45(1): 32-42, 2019 Jan.
Article in English | MEDLINE | ID: mdl-30132727

ABSTRACT

Chronic renal failure (CRF) is among the major health problems that could lead to increased morbidity and mortality among population. 'Nutraceuticals' is an emerging field for natural agents from plant foods that could reduce the progression of such disease. Many newly developed drugs are having bioavailability problems owing to their water insolubility. Liquisolid technique is one of the promising technological approaches to increase solubility and hence, drug absorption. The aim of the present research is to prepare and evaluate the renoprotective effect of the walnut extracts liquisolid formulations in CRF rat model. Saturation solubility study claimed PEG 400 and Tween 20 as good solubilizers for walnut extracts, thus chosen for preparation. The angle of slide was determined for the carrier; microcrystalline cellulose and coating material; silicon dioxide and liquid load factor was evaluated. Eight liquisolid systems were prepared employing 25% and 50% of liquid medication. Their flow and compressibility parameters showed good properties. Dissolution study was more in favor of formulations prepared using PEG 400. Of these, formulation F8 comprising carrier/coat ratio (10:1) and 50% liquid medication, showing superior dissolution properties was selected to perform stability and in-vivo evaluations. Two CRF induced rat groups received F8 at two oral doses (50 and 100 mg/kg). Biochemical and nutritional parameters were compared with both normal and CRF control rats. Results showed improvement of renal function, oxidative stress, antioxidant and inflammatory biomarkers as well as increased appetite and body weight gain on administration of both doses of walnut liquisolid formulation, F8.


Subject(s)
Chemistry, Pharmaceutical/methods , Disease Models, Animal , Drug Carriers/administration & dosage , Juglans , Kidney Failure, Chronic/prevention & control , Plant Extracts/administration & dosage , Animals , Dose-Response Relationship, Drug , Drug Carriers/metabolism , Kidney Failure, Chronic/metabolism , Kidney Failure, Chronic/pathology , Male , Plant Extracts/isolation & purification , Plant Extracts/metabolism , Rats , Rats, Sprague-Dawley , Treatment Outcome
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